obeticholic acid

REMS

Primary biliary cholangitis in patients either without cirrhosis or with compensated cirrhosis and no evidence of portal hypertension (to be used either in combination with ursodeoxycholic acid if experienced an inadequate response to ursodeoxycholic acid or as monotherapy if unable to tolerate ursodeoxycholic acid).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Complete biliary obstruction;
Decompensated cirrhosis or a prior episode of hepatic decompensation;
Compensated cirrhosis with evidence of portal hypertension.

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, peripheral edema

Derm: pruritus, eczema, rash

EENT: oropharyngeal pain

Endo: ↓high-density lipoprotein cholesterol, hypothyroidism

GI: abdominal pain, ascites (worsening), constipation, HEPATIC DECOMPENSATION/FAILURE, ↑liver enzymes, jaundice, VARICEAL BLEEDING

MS: arthralgia

Neuro: fatigue, dizziness, ENCEPHALOPATHY

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Bile acid resins, including cholestyramine, colesevelam, and colestipol may ↓ absorption; give obeticholic acid ≥4 hr before or after bile acid resins.
May ↓ efficacy of warfarin.
May ↑ levels and risk of toxicity of CYP1A2 substrates, including theophylline and tizanidine.
Cyclosporine may exacerbate accumulation of conjugated bile salts; avoid concurrent use.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 10 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg once daily for 3 mo; if adequate reduction in alkaline phosphatase and/or total bilirubin not achieved and tolerating medication, ↑ dose to 10 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Stimulates farnesoid X receptor in the liver and intestine, resulting in decreased synthesis of bile acids from cholesterol and increased transport of bile acids out of the hepatocytes. Overall, the result is a reduction in intracellular hepatocyte concentrations of bile acids.

Therapeutic effects:

Reduction in alkaline phosphatase and total bilirubin concentrations.

Classifications ⬆ ⬇

Therapeutic Classification: none assigned

Pharmacologic Classification: farnesoid X receptor agonists

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly absorbed following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Conjugated in the liver to glycine and tauro conjugates of obeticholic acid (both are active metabolites) that undergo enterohepatic recirculation and conversion by intestinal microbiota back to obeticholic acid that is reabsorbed or excreted in feces. Minimal excretion in urine.

Half-Life: Unknown.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.5 hr	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Advise patient to notify health care professional if signs and symptoms of disease progression or worsening liver function (stomach-area swelling from buildup of fluid; yellowing of skin or whites of eyes; black, tarry, or bloody stools; coughing up or vomiting blood or coffee-grounds vomit; mental changes such as confusion, sleepier than usual or harder to wake up, slurred speech, mood swings, changes in personality), complete biliary obstruction, severe or persistent signs of impaired health (nausea, vomiting, abdominal pain, diarrhea, weight loss, fever and chills, worsening or new fatigue, weakness, loss of appetite, dehydration) occur.
Inform patient of potential for itching. Advise patient to notify health care professional if severe itching causing discomfort, problems sleeping, or interference with daily activities occurs.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Emphasize need for regular laboratory tests to monitor liver function.

Pronunciation ⬆ ⬇

oh-bet-i-KOE-lik AS-id

Code ⬆

NDC Code

69516- Intercept Pharmaceuticals Inc
- 69516-005- Ocaliva
  - 69516-005-30- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (69516-005-30)

69516- Intercept Pharmaceuticals Inc
- 69516-010- Ocaliva
  - 69516-010-30- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (69516-010-30)

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Indications ⬇